TRPV1 agonist approaches for pain management

KR Bley - Vanilloid receptor TRPV1 in drug discovery: targeting …, 2010 - Wiley Online Library
Capsaicin and other naturally occurring pungent molecules have been used for centuries as
topical analgesics to treat a variety of painful conditions. However, only within the last 12 …

TRPV1-targeted drugs in development for human pain conditions

M Iftinca, M Defaye, C Altier - Drugs, 2021 - Springer
The transient receptor potential vanilloid-1 (TRPV1) is a non-specific cation channel known
for its sensitivity to pungent vanilloid compound (ie capsaicin) and noxious stimuli, including …

Medicinal chemistry of the vanilloid (Capsaicin) TRPV1 receptor: current knowledge and future perspectives

L Gharat, A Szallasi - Drug Development Research, 2007 - Wiley Online Library
In peripheral sensory neurons, the vanilloid receptor TRPV1 (transient receptor potential
vanilloid subfamily, member 1) functions as a molecular integrator of painful stimuli …

Transient receptor potential vanilloid 1 channel modulation: a novel approach to pain therapy

VL Korlipara - Current Bioactive Compounds, 2008 - ingentaconnect.com
The TRPV1 vanilloid receptor, first cloned and characterized in 1997, is a non-selective
cation channel expressed in primary sensory neurons, and is a key pain sensor and …

[图书][B] Vanilloid receptor TRPV1 in drug discovery: targeting pain and other pathological disorders

A Gomtsyan, CR Faltynek - 2010 - books.google.com
Examines the emerging therapeutic role of TRPV1 TRPV1 is considered an integrator of
noxious stimuli and therefore may be at a crossroads for pain transmission pathways …

Screening TRPV1 antagonists for the treatment of pain: lessons learned over a decade

J Lázár, L Gharat, N Khairathkar-Joshi… - Expert opinion on …, 2009 - Taylor & Francis
Background: The capsaicin receptor TRPV1, a polymodal nociceptor whose expression is
up-regulated in a number of painful inflammatory disorders, represents a promising …

Therapeutic potential of vanilloid receptor TRPV1 agonists and antagonists as analgesics: Recent advances and setbacks

GY Wong, NR Gavva - Brain research reviews, 2009 - Elsevier
The vanilloid receptor TRPV1 is a homotetrameric, non-selective cation channel abundantly
expressed in the nociceptors (c-fibers). TRPV1 is considered as a highly validated pain …

TRPV1 antagonists

AR Gomtsyan, RG Schmidt, EK Bayburt… - US Patent …, 2011 - Google Patents
BACKGROUND Nociceptors are primary sensory afferent (Cand Aö fibers) neurons that are
activated by a wide variety of noxious stimuli including chemical, mechanical, thermal, and …

Small molecules targeting the vanilloid receptor complex as drug for inflammatory pain

R Planells-Cases, C García-Martínez, M Royo… - 2003 - digital.csic.es
Inflammatory pain is a condition caused by tissue injury and requires efficient drug
treatment. The identification and cloning of the vanilloid receptor TRPV1 represents a …

[HTML][HTML] Identification of a partial and selective TRPV1 agonist CPIPC for alleviation of inflammatory pain

L Dong, Q Zhou, Q Liang, Z Qiao, Y Liu, L Shao… - Molecules, 2022 - mdpi.com
Transient receptor potential vanilloid 1 (TRPV1) is a non-selective cation channel,
predominantly expressed in a subset of peripheral sensory neurons for pain signaling …